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Amisulpride, Sultopride and Sulpiride: Comparison of Conformational and Physico-Chemical Properties

Authors :
Philippe Poirier
François Durant
Laurence Conraux
Audrey Blomme
Mireille Sevrin
Pascal George
Anne Olivier
Jean-Jacques Koenig
Source :
Molecular Modeling and Prediction of Bioactivity ISBN: 9781461368571
Publication Year :
2000
Publisher :
Springer US, 2000.

Abstract

Amisulpride, sultopride and sulpiride (Figure 1) are antagonists of the D2-like dopamine receptors, which are members of a large family of receptors that interact with specific intracellular signalling pathways through coupling with G proteins. These compounds are substituted benzamides and present a high degree of selectivity for D2 and D3 versus D1 and D4 dopaminergic receptor subtypes. Amisulpride, sultopride and sulpiride respectively present decreasing in vitro affinities for the D2 receptor (IC50 = 27, 120 and 181 nM) and the D3 receptor (IC50 = 3.6, 4.8 and 17.5 nM).

Details

ISBN :
978-1-4613-6857-1
ISBNs :
9781461368571
Database :
OpenAIRE
Journal :
Molecular Modeling and Prediction of Bioactivity ISBN: 9781461368571
Accession number :
edsair.doi...........806e3cc4f25beea7e99ee52e5febf054
Full Text :
https://doi.org/10.1007/978-1-4615-4141-7_97